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ORGANIZATION OF CLASS

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A high level of glucose stimulates an increase in insulin release from β cells of the pancreas. Insulin then drives carbohydrate into cells. Patients who have high glucose levels in their blood are said to have diabetes mellitus.

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Of course, you remember that diabetes mellitus is divided into two groups: type I (insulin dependent) and type II (insulin resistance). These distinctions are important for pharmacology because they make it easier to remember the mechanism of action of the drugs used to treat diabetes mellitus.

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As an aside, there is another form of diabetes that students sometimes confuse with diabetes mellitus and that is diabetes insipidus. Diabetes insipidus is a disorder of water and sodium balance. Generally, if someone says diabetes, they mean the sugar-related (mellitus) disease and not diabetes insipidus.

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But let’s return to the topic at hand.

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Type I diabetes is related to loss of insulin-secreting cells in the pancreas. Type II diabetes is related to target cell resistance to the action of insulin.

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This, of course, is somewhat simplified. An endocrinologist would cringe. Patients with type I diabetes are dependent on an exogenous (outside the body) source of insulin. This disorder generally appears in childhood; hence the former term for it is juvenile diabetes. Type II diabetes has been called adult-onset. It appears to have a genetic basis, and patients are often obese. Patients with type II diabetes are treated with oral agents that lower blood glucose (hypoglycemics) and with insulin.

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So, that said, we should organize our drugs into insulins and the oral hypoglycemic agents.

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INSULINS

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Insulin is a small protein that is synthesized and secreted by the β cells of the pancreas. Insulin for replacement therapy can be isolated from animal sources. Human insulin is made using recombinant DNA technology.

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INSULIN must be administered by injection.

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All peptides are degraded by enzymes in the gastrointestinal (GI) tract, so it is not possible to administer insulin by the oral route. Given intravenously, it has a half-life of less than 10 minutes (short). Therefore, it is administered subcutaneously.

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The most common adverse effect of insulin is hypoglycemia.

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I hope that this is intuitively obvious.

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Insulin preparations vary in their time to onset and duration of action.

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The onset and duration of action of the insulin preparations are controlled by the size and composition of the crystals in the particular insulin preparation.

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Types of Insulin Preparations

Rapid onset and short duration

 aspart

 lispro

 insulin glulisine

 crystalline zinc insulin (regular)

 prompt insulin (SEMILENTE)

Intermediate onset and duration

 isophane insulin (NPH)

 insulin zinc (LENTE, mixture of semilente and ultralente)

Prolonged duration

 protamine zinc insulin

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